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Author (up) Jakubikova, J.; Duraj, J.; Hunakova, L.; Chorvath, B.; Sedlak, J. file  url
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  Title PK11195, an isoquinoline carboxamide ligand of the mitochondrial benzodiazepine receptor, increased drug uptake and facilitated drug-induced apoptosis in human multidrug-resistant leukemia cells in vitro Type Journal Article
  Year 2002 Publication Neoplasma Abbreviated Journal Neoplasma  
  Volume 49 Issue 4 Pages 231-236  
  Keywords Antineoplastic Agents/*metabolism/*pharmacology/toxicity; Apoptosis/*drug effects; Biological Transport; Carcinoma/drug therapy/metabolism; Daunorubicin/*metabolism/toxicity; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Drug Synergism; Female; Fluoresceins/metabolism; Fluorescent Dyes/metabolism; HL-60 Cells; Humans; Isoquinolines/metabolism/*pharmacology; Leukemia, Myeloid/*drug therapy/metabolism; Ligands; Mitochondrial Proteins/metabolism; Ovarian Neoplasms/drug therapy/metabolism; P-Glycoprotein/genetics; Receptors, GABA-A/metabolism; Tumor Cells, Cultured  
  Abstract The isoquinoline peripheral benzodiazepine receptor ligand PK11195 increased drug (daunomycin)- and fluorochrome (calcein-AM) uptake and induced apoptosis detected by flow cytometry (FCM) technique, DNA electrophoretic analysis and poly(ADP-ribose) polymerase (PARP) cleavage in human multidrug-resistant myeloid leukemia (BL-60/VCR) and ovarian carcinoma (A2780/ADR) cells in vitro. The position of PK11195 with respect to drug-resistance modulator (DRM) efficiency, compared to the reference DRMs with the aid of FCM technique, was as follows: PSC833 > verapamil > PK11195 > vincristine. Our data show up to now not indicated observation that PK11195 possesses multidrug resistance modulating activity.  
  Call Number Serial 398  
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